盐酸纳曲酮片（Naltrexone Hydrochloride Tablets）

盐酸纳曲酮片（Naltrexone Hydrochloride Tablets） 盐酸纳曲酮片(Naltrexone Hydrochloride Tablets) 盐酸纳曲酮片(盐酸纳曲酮片) 本品主要成份其化学名称:17环丙基甲基- 4，与α-环氧- 3d -二羟基吗喃- 6 -酮盐酸盐。 【性状】 本品为白色或类白色片。 【药理毒理】 药理学 纳曲酮是阿片受体桔抗剂，药效学与纳洛酮的作用相似，能明显的减弱或完全阻断阿片受体，甚至反转由静脉注射阿片类药物所产生的作用。能解除其对阿片的身体依赖性，使已戒断阿片瘾者保持正常生活。本品口服有效，而且作用维持时间较长。本品不产生躯体或精神依赖性。 毒理学 本品对大鼠2年的致癌研究，在雄鼠间皮瘤和两性中血管源性肿瘤的数目稍有增加但除雌性血管瘤稍有增加外，肿瘤的发生都在对照组的范围内。 【药代动力学】 纳曲酮口服后主要消除途径是大量被肝脏代谢，约占有吸收量的95%变为几种代谢产物，其中主要的活性代谢产物是6-B纳曲醇(6 - B -纳曲醇)，其药理作用也是阻断阿片受体。一个次要的代谢物是2羟 基- 3 -甲氧基-两纳曲醇。纳曲酮及其代谢物主要经肾脏排出，原形由尿中排出的不到口服剂量的1%，由尿中排出的原形药物和结合的6-B纳曲醇约为口服剂量的38%。从药代动力学来看，本品及其代谢物能发生肝肠循环。 给24名男性志愿者服用50mg纳曲酮后，纳曲酮及其主要代谢产物6-B纳曲醇的Cmax分别为8.6和99.3mg,ml。在50,200mg用量之间纳曲酮和6-B纳曲醇的Cmax和AUC呈比例的增加。Tmax约1小时。纳曲酮和6-B纳曲醇的消除T1,2分别为3.9和12.9小时。其平均消除T1,2和Tmax与用量无关。纳曲酮不在体内蓄积。由于T1,2长，两纳曲醇的血浓度在长期给药时可增加40%。 体内纳曲酮的总清除率为1.5l /分(相当肝血流)。其肾清除率为127ml /分，完全由肾小球滤过。两纳曲醇的肾清除率为283ml /分，推测有肾小管分泌机制。 纳曲酮静注后的分布容积为1350升纳曲酮在治疗剂量范围内约有21%与血浆蛋白结合。 【适应症】 盐酸纳曲酮主要用于对已解除阿片类药物毒瘾者的康复期辅助治疗，使戒除阿片瘾者能维正常生活，防止或减少复吸。 【用法用量】 纳曲酮治疗必须在纳洛酮诱发呈阴性时才能实行。所以必须按下列原则用药: 1、本品需在阿片瘾者戒断后7,10天后使用。戒断需经检查患者尿样证实再以纳洛酮诱发，进一步确定不存在阿片依赖性。 2、纳洛酮诱发试验:针筒内吸入盐酸纳洛酮0.8mg先静脉注射盐酸 纳洛酮0.2mg、观察30秒钟看患者是否有阿片依赖性，若呈阴性反 应，继续静注0.6mg，并观察20,30分钟，无症状者可给予治疗。 3、纳洛酮治疗可有以下几种:每个工作日口服50mg，周六给 100mg;隔日给100mg或每3天给150mg，疗程可持续半年。 【不良反应】 1、纳曲酮的每日用量达到300mg时可引起肝细胞损害。 2、除肝损害外，不良反应发生率在10%以上的反应有:睡眠困难、 焦虑、易激动、腹痛/痉挛、恶心和/或呕吐、关节肌肉痛、头痛。 3、不良反应发生率在10%以下的反应有:食欲不振、腹泻、便秘、 口渴、头晕。 4、在1%以下的不良反应有: Respiratory system: nasal congestion, itching, runny nose, sore throat, excessive mucus, hoarseness, cough, shortness of breath. Cardiovascular system: nasal bleeding, phlebitis, edema, elevated blood pressure, nonspecific ECG changes, palpitation and tachycardia. Gastrointestinal tract: excessive gas, hematochezia, diarrhea and ulcer. Muscular bone: pain and tremors in the shoulders, legs and knees. Skin: oily skin, itching, acne, lip herpes. Genitourinary system: increased urination discomfort, decreased libido. Mental aspects: depression, forgetting, fatigue, restlessness, confusion, hallucinations, nightmares. [taboo] The disabled naltrexone: 1. Opioid analgesics. 2. Patients with opioid addiction who have not been abstinent. 3, suddenly disable opioid patients. 4, naltrexone induced failure patients. 5, opioid positive urine test. 6. It is not clear whether the product is cross allergic to naloxone or other opioid containing vitamins. 7, acute hepatitis or liver failure of individual. [matters needing attention] 1, this product has liver toxicity, can cause elevation of transaminase. By 5 times liver toxicity of the clinical dose of only the amount used, so mild impairment of liver function should be used with caution. 2, to avoid withdrawal symptoms or withdrawal symptoms worsened, patients in the application of naltrexone before there should be at least 7 to 10 days the body is indeed non opioid. 3, application of this product before or after the application should regularly check the liver function, the best monthly check 1 times. [pregnant women and lactating women] This product belongs to the pregnancy risk C class medicine. The experiment proved that the dosage of 140 times the clinical dose (about 100mg/kg) could kill the embryo in rabbits and rats, and the proportion of sham pregnancy and the conception rate of female mice were significantly increased in rats. But there are no reports of fertility effects in humans. It is not known whether this product can be removed from human milk. Whether or not it affects the course of labor is unknown. Therefore, pregnant women and lactating women should use this product carefully. [children medication] The safety of this product for individuals under 18 years of age has not yet been determined. [medication for elderly patients] [drug interaction] This product may interfere with the therapeutic effects of opioids, which should be avoided when opioid analgesics are used. [drug overdose] No one has ever used excessive experience. Only 1 study shows that daily naltrexone 800mg, for 1 weeks without any toxicity. In mice, rats and guinea pigs, the oral doses of LD50 were 1.100 + 96mg/kg, (1.450 + 265) mg/kg and 1.490 + 102mg/kg. The causes of acute death in mice, rats and dogs are clonic tetanic convulsions and respiratory failure. Naltrexone treatment because of the lack of experience excessive, it should be prepared to symptomatic treatment. [specifications] Tablet: 5mg [YSNQTP] The previous page, the last page, the front page